Oestrogenic activity of mimosine on MCF-7 breast cancer cell line through the ERα-mediated pathway

Akm Moyeenul Huq1, Lam Kok Wai1, Kamal Rullah1

  • 1Drug and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur, Malaysia.

Insights

Mimosine, a plant compound, exhibits estrogenic activity by interacting with the estrogen receptor alpha (ERα). This suggests potential as a safer alternative for postmenopausal symptom treatment compared to traditional hormone replacement therapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Hormone replacement therapy (HRT) is a common treatment for postmenopausal symptoms.
  • HRT carries risks, including increased breast and endometrial cancer.
  • Safer alternatives are needed for managing menopausal symptoms.

Purpose of the Study:

  • To evaluate the estrogenic potential of mimosine, a plant-derived compound.
  • To investigate mimosine's effects on estrogen receptor alpha (ERα) activity in MCF-7 cells using in silico methods.

Main Methods:

  • In silico modeling, including docking and molecular dynamics simulations, was used to assess ERα binding.
  • Cell viability, proliferation, and ERα-dependent gene expression (TFF1, PGR) were measured.
  • Coactivator (SRC1) recruitment and binding energy calculations were performed.

Main Results:

  • Mimosine demonstrated significant cellular viability and proliferation, comparable to 17β-estradiol.
  • Mimosine increased ERα-SRC1 coactivator activity and induced expression of ERα-dependent genes TFF1 and PGR.
  • Molecular modeling showed strong binding affinity of mimosine to the ERα ligand-binding domain.

Conclusions:

  • Mimosine exhibits estrogenic activity, interacting with ERα.
  • The findings suggest mimosine as a potential candidate for developing novel therapies for postmenopausal symptoms.
  • Further research is warranted to explore mimosine's therapeutic applications and safety profile.

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